基于寡肽转运蛋白的氟苯尼考肠吸收特性研究

doi:10.11843/j.issn.0366-6964.2023.03.035

Abstract

Abstract: The aim of this study was to investigate the intestinal absorption characteristics of florfenicol (FF) at different concentrations, and to explore the effect of oligopeptide transporter on intestinal absorption of florfenicol. The content of florfenicol in the perfusion samples was determined by high performance liquid chromatography (HPLC), and the in vivo circulation pass perfusion model was established to investigate the effect of different concentrations of drugs on the absorption rate of florfenicol; The effect of PepT1 on florfenicol uptake was investigated by the typical substrate of oligopeptide transporter 1 (PepT1), glycine sarcosine, and the drug absorption rate constant (K_a) and effective permeability coefficient (P_eff) of florfenicol were calculated. he results show that the accuracy and precision of the established method for determination of FF content meet the detection requirements. The K_a (μg·h^-1·cm^-2) values at low (50 μg·mL^-1), medium (75 μg·mL^-1) and high (100 μg·mL^-1) concentrations were 1.48±0.02, 1.73±0.14 and 1.90±0.07, respectively, and there were significant differences between low and medium concentration groups (P<0.05). The effective permeability coefficient P_eff (×10² cm·h^-1) was 84.12±2.40, 101.28±4.57, 110.64±5.70, respectively, with significant differences among the three groups (P<0.05). The K_a and P_eff absorbed by FF across the gut increased with increasing concentration in the concentration range used in the experiment. The P_eff (×10² cm·h^-1) value was 97.2±5.30 after the addition of high concentration (100 μg·mL^-1) glycine sarcosine (GlySar), which was significantly different from that of the non-addition group. The absorption of florfenicol decreased significantly after the addition of PepT1 typical substrate. The above experimental results suggest that the absorption mechanism of florfenicol is not only simple diffusion, and PepT1 as an active transporter participates in the trans-intestinal absorption process of florfenicol.

Key words: florfenicol, intestinal absorption, in vivo circulation pass perfusion model, oligopeptide transporters

CLC Number:

S859.796

CHEN Yang, WANG Yueli, CHEN Shiqi, LI Nanxin, ZHANG Wei, SHU Gang, XU Funeng, LI Haohuan, LIN Juchun, FU Hualin. Intestinal Absorption Characteristics of Florfenicol based on Oligopeptide Transporters[J]. Acta Veterinaria et Zootechnica Sinica, 2023, 54(3): 1240-1248.

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Intestinal Absorption Characteristics of Florfenicol based on Oligopeptide Transporters

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